GPi688
GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively. GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia.
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- CAS. Nr.: 918902-32-6
- Formel: C19H18ClN3O4S
- Molecular Weight:419.88
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
IC50: 19 nM (human liver GPa), 61 nM (rat liver GPa), 12 nM (human skeletal muscle GPa)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
1.1 μM
Compound: 33
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Inhibition of glucose output in glucagon challenged primary rat hepatocytes
Inhibition of glucose output in glucagon challenged primary rat hepatocytes
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[PMID: 17095214] |
Chemical Information
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CAS. Nr. 918902-32-6
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Molecular Weight 419.88
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Formel C19H18ClN3O4S
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SMILES
O=C(C1=CC(C=C(Cl)S2)=C2N1)NC3C(N(C[C@@H](O)CO)C4=C(C=CC=C4)C3)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Freeman S, et al. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br J Pharmacol. 2006;149(6):775-785. [Content Brief]
[2]. Poucher SM, et al. An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br J Pharmacol. 2007;152(8):1239-1247. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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